| 高质量盐酸多奈哌齐的制备方法 |
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| 引用本文： | 冯建鹏,祝传宝,胡丽娜,王伟.高质量盐酸多奈哌齐的制备方法[J].河北化工,2012(9):12-13,16. |
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| 作者姓名： | 冯建鹏 祝传宝 胡丽娜 王伟 |
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| 作者单位： | 扬子江药业集团江苏海慈生物药业有限公司研发部,江苏泰州225321 |
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| 基金项目： | 国家“十二五”重大新药创制项目（2012ZX09201101-003） |
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| 摘 要： | 提供了一条较为简洁的盐酸多奈哌齐合成路线,即以5,6-二甲氧基-2-(4-哌啶基甲基)-2,3-二氢-1H-茚酮为起始原料,PtO2催化氢化将吡啶还原为哌啶衍生物,以刘卡特-瓦拉赫反应为关键反应将胺基苄基取代制得盐酸多奈哌齐。再经过成盐和精制,以四步反应,69%的总收率得到了高质量的药用盐酸多奈哌齐。
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| 关 键 词： | 盐酸多奈哌齐 阿尔茨海默病 刘卡特-瓦拉赫反应 精制 |
Preparation Method of High Quality Donepezil hydrochloride |
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| FENG Jian-peng,ZHU Chuan-bao,HU Li-na,WANG Wei.Preparation Method of High Quality Donepezil hydrochloride[J].Hebei Chemical Engineering and Industry,2012(9):12-13,16. |
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| Authors: | FENG Jian-peng ZHU Chuan-bao HU Li-na WANG Wei |
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| Affiliation: | (Research and Development Department,Yangtze River Pharmaceutical Group Jiangsu Haici Biological Pharmaceutical Co.,Ltd,Taizhou 225321,China) |
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| Abstract: | To provide a concise synthetic route of donepezil hydrochloride.Firstly,to choose 5,6-dimethoxy-2-（4-piperidinyl methylene）-2,3-dihydro-1H-inden-1-one as the starting material,to reduce pyridine to piperidine derivative,by PtO2 hydrogenization.Secondly to prepare donepezil hydrochloride,by the key Leuckart-Wallach reaction.Finally,by salification and refination,to obtain the high quality pharmaceutical grade donepezil hydrochloride by four step reaction with a overall yield of 69%. |
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| Keywords: | donepezil hydrochloride aldo-keto reductase inhibitor Leuckart-Wallach reaction refination |
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